A High-Throughput Dose-Response Cellular Thermal Shift Assay for Rapid Screening of Drug Target Engagement in Living Cells, Exemplified Using SMYD3 and IDO1

The Cellular Thermal Shift Assay: A Novel Biophysical Assay for In Situ Drug Target Engagement and Mechanistic Biomarker Studies

(2016) Daniel Martinez Molina et al.   Annual Review of Pharmacology and Toxicology

Design and synthesis of N -(5-chloro-2,4-dihydroxybenzoyl)-( R )-1,2,3,4-tetrahydroisoquinoline-3-carboxamides as novel Hsp90 inhibitors

(2016) Chuanpeng Liang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil

(2016) Helena Almqvist et al.   Nature Communications

Compounds from the marine sponge Cribrochalina vasculum offer a way to target IGF-1R mediated signaling in tumor cells

(2016) Ana Zovko et al.   Oncotarget

CETSA: a target engagement assay with potential to transform drug discovery

(2015) Annika Jenmalm Jensen et al.   Future Medicinal Chemistry

A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models

(2015) Elayne Chan-Penebre et al.   Nature Chemical Biology

Targeting the MLL complex in castration-resistant prostate cancer

(2015) Rohit Malik et al.   NATURE MEDICINE

Thermal proteome profiling monitors ligand interactions with cellular membrane proteins

(2015) Friedrich B M Reinhard et al.   NATURE METHODS

Target engagement and drug residence time can be observed in living cells with BRET

(2015) Matthew B. Robers et al.   Nature Communications

Identification of a new class of natural product MDM2 inhibitor: In vitro and in vivo anti-breast cancer activities and target validation

(2015) Jiang-Jiang Qin et al.   Oncotarget

Assessing the Efficacy of Mdm2/Mdm4-Inhibiting Stapled Peptides Using Cellular Thermal Shift Assays

(2015) Ban Xiong Tan et al.   Scientific Reports

Discovery and characterization of novel small-molecule inhibitors targeting nicotinamide phosphoribosyltransferase

(2015) Tian-Ying Xu et al.   Scientific Reports

Hsp90 Is a Novel Target Molecule of CDDO-Me in Inhibiting Proliferation of Ovarian Cancer Cells

(2015) Dong-Jun Qin et al.   PLoS One

EZH2 Inhibitor Efficacy in Non-Hodgkin’s Lymphoma Does Not Require Suppression of H3K27 Monomethylation

(2014) William D. Bradley et al.   CHEMISTRY & BIOLOGY

Intracellular drug concentration and disposition – The missing link?

(2014) Michael M. Hann et al.   METHODS

NQO2 Is a Reactive Oxygen Species Generating Off-Target for Acetaminophen

(2014) Teemu P. Miettinen et al.   MOLECULAR PHARMACEUTICS

Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy

(2014) Kilian V. M. Huber et al.   NATURE

MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool

(2014) Helge Gad et al.   NATURE

SMYD3 links lysine methylation of MAP3K2 to Ras-driven cancer

(2014) Pawel K. Mazur et al.   NATURE

The cellular thermal shift assay for evaluating drug target interactions in cells

(2014) Rozbeh Jafari et al.   Nature Protocols

Lessons learned from the fate of AstraZeneca's drug pipeline: a five-dimensional framework

(2014) David Cook et al.   NATURE REVIEWS DRUG DISCOVERY

BM-1197: A Novel and Specific Bcl-2/Bcl-xL Inhibitor Inducing Complete and Long-Lasting Tumor Regression In Vivo

(2014) Longchuan Bai et al.   PLoS One

Tracking cancer drugs in living cells by thermal profiling of the proteome

(2014) M. M. Savitski et al.   SCIENCE

Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay

(2013) D. M. Molina et al.   SCIENCE

Colloidal Aggregation Affects the Efficacy of Anticancer Drugs in Cell Culture

(2012) Shawn C. Owen et al.   ACS Chemical Biology

Smyd3 regulates cancer cell phenotypes and catalyzes histone H4 lysine 5 methylation

(2012) Glenn S. Van Aller et al.   Epigenetics

Heat-shock-induced cellular responses to temperature elevations occurring during orthopaedic cutting

(2012) E. B. Dolan et al.   Journal of the Royal Society Interface

Purification and kinetic characterization of human indoleamine 2,3-dioxygenases 1 and 2 (IDO1 and IDO2) and discovery of selective IDO1 inhibitors

(2011) David Meininger et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

Can the flow of medicines be improved? Fundamental pharmacokinetic and pharmacological principles toward improving Phase II survival

(2011) Paul Morgan et al.   DRUG DISCOVERY TODAY

Structural and Functional Profiling of the Human Histone Methyltransferase SMYD3

(2011) Kenneth W. Foreman et al.   PLoS One